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    Guanidine derivatives
    2.
    发明授权
    Guanidine derivatives 失效
    胍衍生物

    公开(公告)号：US07544691B2

    公开(公告)日：2009-06-09

    申请号：US10570517

    申请日：2004-09-03

    申请人： Volker Breu ,  Anja Fecher ,  Heinz Fretz ,  Thomas Giller ,  Kurt Hilpert ,  Olivier Valdenaire

    发明人： Volker Breu ,  Anja Fecher ,  Heinz Fretz ,  Thomas Giller ,  Kurt Hilpert ,  Olivier Valdenaire

    IPC分类号： A61K31/517

    CPC分类号： C07D239/84 ,  A61K31/517 ,  C07D239/70

    摘要： The invention relates to the guanine derivatives of general formula (I), and to hydrates or solvents thereof, for use as neuropeptide FF receptor antagonists in the treatment of pains and hyperalgesia, of withdrawal symptoms of addiction to alcohol, psychotropic drugs or nicotine and in the prevention of or recovery from these addictions, for the regulation of insulin release, food intake, memory functions, blood pressure, electrolyte and energy metabolism, and in the treatment of urinary incontinence

    摘要翻译： 本发明涉及通式（I）的鸟嘌呤衍生物及其水合物或溶剂，用作治疗痛苦和痛觉过敏的神经肽FF受体拮抗剂，对酒精，精神药物或尼古丁成瘾的戒断症状以及 预防或恢复这些成瘾，调节胰岛素释放，食物摄入，记忆功能，血压，电解质和能量代谢以及治疗尿失禁

    Guanidine derivatives and their use as neuropeptide FF receptor antagonists
    3.
    发明授权
    Guanidine derivatives and their use as neuropeptide FF receptor antagonists 失效
    胍衍生物及其作为神经肽FF受体拮抗剂的用途

    公开(公告)号：US07727979B2

    公开(公告)日：2010-06-01

    申请号：US10549685

    申请日：2004-03-22

    申请人： Eva Caroff ,  Matthias Steger ,  Oliver Valdenaire ,  Anja Fecher ,  Volker Breu ,  Kurt Hilpert ,  Heinz Fretz ,  Thomas Giller

    发明人： Eva Caroff ,  Matthias Steger ,  Oliver Valdenaire ,  Anja Fecher ,  Volker Breu ,  Kurt Hilpert ,  Heinz Fretz ,  Thomas Giller

    IPC分类号： A01N43/00 ,  A01N43/46 ,  A61K31/55 ,  A01N43/42 ,  A61K31/44 ,  A01N43/78 ,  A61K31/425 ,  A01N37/52 ,  A61K31/155 ,  C07D277/60 ,  C07D277/62 ,  C07D277/82

    CPC分类号： C07D277/60 ,  A61K31/428 ,  A61K31/429 ,  A61K31/437 ,  C07D277/82 ,  C07D417/04 ,  C07D513/04

    摘要： The invention relates to guanidine derivatives of formula (I) where: A represents a chain of 3-6 carbon atoms, one of which can be replaced by —N(R′)— or —O— and R′ is H or a substituent; the ring skeleton only contains both double bonds of the thiazole component; the pharmaceutically-acceptable acid addition salts of basic compounds of formula (I), the pharmaceutically-acceptable salts of compounds of formula (I), comprising acid groups, with bases, the pharmaceutically-acceptable esters of hydroxy or carboxyl group containing compounds of formula (I) and the solvates or hydrates thereof, which exhibit a neuropeptide FF receptor antagonist effect. The above are suitable for the treatment of pain and hyperalgesia, withdrawal symptoms in alcohol, psychotropic and nicotine dependencies, for improvement or cure of said dependencies, for regulation of insulin excretion, food intake, memory functions, blood pressure, electrolyte and energy management and for treatment of urinary incontinence. The above can be produced using generally used methods and processed to give medicaments.

    摘要翻译： 本发明涉及式（I）的胍衍生物，其中：A表示3-6个碳原子的链，其中一个可以被-N（R'） - 或-O-代替，R'是H或取代基 ; 环骨架仅含有噻唑组分的双键; 式（I）的碱性化合物的药学上可接受的酸加成盐，包含酸基的式（I）化合物与碱的药学上可接受的盐，含有羟基或羧基的式 （I）及其溶剂合物或水合物，其表现出神经肽FF受体拮抗剂作用。 以上适用于治疗疼痛和痛觉过敏，酒精戒断症状，​​精神药物和尼古丁依赖性，用于改善或治愈所述依赖性，调节胰岛素排泄，食物摄取，记忆功能，血压，电解质和能量管理以及 用于治疗尿失禁。 上述可以使用通常使用的方法制备并加工以得到药物。

    Guanidine derivatives and their use as neuropeptide ff receptor antagonists
    4.
    发明申请
    Guanidine derivatives and their use as neuropeptide ff receptor antagonists 失效
    胍衍生物及其作为神经肽ff受体拮抗剂的用途

    公开(公告)号：US20060194788A1

    公开(公告)日：2006-08-31

    申请号：US10549685

    申请日：2004-03-22

    申请人： Eva Caroff ,  Matthias Steger ,  Oliver Valdenaire ,  Anja Fecher ,  Volker Breu ,  Kurt Hilpert ,  Heinz Fretz ,  Thomas Giller

    发明人： Eva Caroff ,  Matthias Steger ,  Oliver Valdenaire ,  Anja Fecher ,  Volker Breu ,  Kurt Hilpert ,  Heinz Fretz ,  Thomas Giller

    IPC分类号： A61K31/55 ,  A61K31/4745 ,  A61K31/43

    CPC分类号： C07D277/60 ,  A61K31/428 ,  A61K31/429 ,  A61K31/437 ,  C07D277/82 ,  C07D417/04 ,  C07D513/04

    摘要： The invention relates to guanidine derivatives of formula (I) where: A represents a chain of 3-6 carbon atoms, one of which can be replaced by —N(R′)— or —O— and R′ is H or a substituent; the ring skeleton only contains both double bonds of the thiazole component; the pharmaceutically-acceptable acid addition salts of basic compounds of formula (I), the pharmaceutically-acceptable salts of compounds of formula (I), comprising acid groups, with bases, the pharmaceutically-acceptable esters of hydroxy or carboxyl group containing compounds of formula (I) and the solvates or hydrates thereof, which exhibit a neuropeptide FF receptor antagonist effect. The above are suitable for the treatment of pain and hyperalgesia, withdrawal symptoms in alcohol, psychotropic and nicotine dependencies, for improvement or cure of said dependencies, for regulation of insulin excretion, food intake, memory functions, blood pressure, electrolyte and energy management and for treatment of urinary incontinence. The above can be produced using generally used methods and processed to give medicaments.

    摘要翻译： 本发明涉及式（I）的胍衍生物，其中：A表示3-6个碳原子的链，其中一个可以被-N（R'） - 或-O-代替，R'是H或取代基 ; 环骨架仅含有噻唑组分的双键; 式（I）的碱性化合物的药学上可接受的酸加成盐，包含酸基的式（I）化合物与碱的药学上可接受的盐，含有羟基或羧基的式 （I）及其溶剂合物或水合物，其表现出神经肽FF受体拮抗剂作用。 以上适用于治疗疼痛和痛觉过敏，酒精戒断症状，​​精神药物和尼古丁依赖性，用于改善或治愈所述依赖性，调节胰岛素排泄，食物摄取，记忆功能，血压，电解质和能量管理以及 用于治疗尿失禁。 上述可以使用通常使用的方法制备并加工以得到药物。

    Pyrrolidone carboxamides
    5.
    发明授权
    Pyrrolidone carboxamides 失效
    吡咯烷酮甲酰胺

    公开(公告)号：US07067549B2

    公开(公告)日：2006-06-27

    申请号：US10500604

    申请日：2002-12-27

    申请人： Markus Isler ,  Thomas Giller ,  Günter Schwalm ,  Matthias Steger ,  Kurt Hilpert ,  Oliver Valdenaire ,  Volker Breu

    发明人： Markus Isler ,  Thomas Giller ,  Günter Schwalm ,  Matthias Steger ,  Kurt Hilpert ,  Oliver Valdenaire ,  Volker Breu

    IPC分类号： A61K31/403 ,  C07D209/82

    CPC分类号： C07D207/277 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14

    摘要： Pyrrolidone carboxamides of formula (I) where R2=a group of formula (a) or (b), R5=phenyl, heteroalkyl, aryloxy, alkoxy, alkanoyl or —NR6R7 and R1, X, R3, R4, R6 and R7 have the meanings given in the description and the claims, pharmaceutically applicable acid addition salts with basic compounds of formula (I), pharmaceutically applicable salts of acid compounds of formula (I) with bases, pharmaceutically applicable esters of hydroxy- or carboxy-group containing compounds of formula (I) and hydrates and solvates thereof, inhibit the interaction of neuropeptide Y (NPY) with one of the neuropeptide receptor subtypes (NPY-Y5) and are particularly suitable for the prevention and treatment of arthritis, diabetes and especially eating disorders and obesity. The above can be produced by known methods and converted into a galenic dosage form.

    摘要翻译： 式（I）的吡咯烷酮甲酰胺其中R 2 =式（a）或（b）的基团，R 5 =苯基，杂烷基，芳氧基，烷氧基，烷酰基或 R 6，R 7，R 12，R 11，R 4，R 4， >，R 6和R 7具有在说明书和权利要求书中给出的含义，药学上适用的与式（I）的碱式化合物的酸加成盐，药学上适用的盐 具有碱的式（I）酸化合物，含有羟基或羧基的式（I）化合物的药学上适用的酯及其水合物和溶剂合物抑制神经肽Y（NPY）与神经肽受体亚型之一的相互作用 NPY-Y5），特别适用于预防和治疗关节炎，糖尿病，特别是进食障碍和肥胖症。 上述可以通过已知方法制备并转化成盖仑剂型。

    Pyrrolidone carboxamides
    6.
    发明申请
    Pyrrolidone carboxamides 失效
    吡咯烷酮甲酰胺

    公开(公告)号：US20050192292A1

    公开(公告)日：2005-09-01

    申请号：US10500604

    申请日：2002-12-27

    申请人： Markus Isler ,  Thomas Giller ,  Gunter Schwaim ,  Matthias Steger ,  Kurt Hilpert ,  Oliver Valdenaire ,  Volker Breu

    发明人： Markus Isler ,  Thomas Giller ,  Gunter Schwaim ,  Matthias Steger ,  Kurt Hilpert ,  Oliver Valdenaire ,  Volker Breu

    IPC分类号： C07D207/26 ,  C07D207/277 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  A61K31/506 ,  A61K31/403 ,  C07D43/02 ,  C07D43/14

    CPC分类号： C07D207/277 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14

    摘要： Pyrrolidone carboxamides of formula (I) where R2=a group of formula (a) or (b), R5=phenyl, heteroalkyl, aryloxy, alkoxy, alkanoyl or —NR6R7 and R1, X, R3, R4, R6 and R7 have the meanings given in the description and the claims, pharmaceutically applicable acid addition salts with basic compounds of formula (I), pharmaceutically applicable salts of acid compounds of formula (I) with bases, pharmaceutically applicable esters of hydroxy- or carboxy-group containing compounds of formula (I) and hydrates and solvates thereof, inhibit the interaction of neuropeptide Y (NPY) with one of the neuropeptide receptor subtypes (NPY-Y5) and are particularly suitable for the prevention and treatment of arthritis, diabetes and especially eating disorders and obesity. The above can be produced by known methods and converted into a galenic dosage form.

    摘要翻译： 式（I）的吡咯烷酮甲酰胺其中R 2 =式（a）或（b）的基团，R 5 =苯基，杂烷基，芳氧基，烷氧基，烷酰基或 R 6，R 7，R 12，R 11，R 4，R 4， >，R 6和R 7具有在说明书和权利要求书中给出的含义，药学上适用的与式（I）的碱式化合物的酸加成盐，药学上适用的盐 具有碱的式（I）酸化合物，含有羟基或羧基的式（I）化合物的药学上适用的酯及其水合物和溶剂合物抑制神经肽Y（NPY）与神经肽受体亚型之一的相互作用 NPY-Y5），特别适用于预防和治疗关节炎，糖尿病，特别是进食障碍和肥胖症。 上述可以通过已知方法制备并转化成盖仑剂型。

    Pyrazolidinedione derivatives
    7.
    发明申请
    Pyrazolidinedione derivatives 审中-公开
    吡唑烷二酮衍生物

    公开(公告)号：US20070037846A1

    公开(公告)日：2007-02-15

    申请号：US10562623

    申请日：2004-06-16

    申请人： Heinz Fretz ,  Thomas Giller ,  Kurt Hilpert ,  Olivier Houille ,  Markus Riederer ,  Oliver Valdenaire

    发明人： Heinz Fretz ,  Thomas Giller ,  Kurt Hilpert ,  Olivier Houille ,  Markus Riederer ,  Oliver Valdenaire

    IPC分类号： A61K31/4152 ,  A61K31/4709 ,  A61K31/416

    CPC分类号： A61K31/4152 ,  A61K31/416 ,  A61K31/4709

    摘要： The present invention relates to compounds of alkylidene pyrazolidinedione derivatives, which are effective platelet ADP receptor antagonists that prevent platelet aggregation and thrombosis. Thus, the present invention also relates to pharmaceutical compositions that contain the compounds as well as methods of preventing or treating peripheral, visceral, hepatic, renal, cardio- and cerebro-vascular diseases and conditions that are associated with platelet aggregation, including thrombosis, in humans and other mammals. The present invention further provides a process for manufacturing the alkylidene pyrazolidinedione derivatives.

    摘要翻译： 本发明涉及亚烷基吡唑烷二酮衍生物的化合物，其是有效的血小板聚集和血栓形成的血小板ADP受体拮抗剂。 因此，本发明还涉及含有化合物的药物组合物以及预防或治疗外周，内脏，肝，肾，心脑血管疾病和与血小板聚集相关的病症的方法，包括血栓形成 人类和其他哺乳动物。 本发明还提供了制备亚烷基吡唑烷二酮衍生物的方法。

    RESINIFERATOXIN SOLUTION
    8.
    发明申请
    RESINIFERATOXIN SOLUTION 审中-公开
    RESINIFERATOXIN溶液

    公开(公告)号：US20150190509A1

    公开(公告)日：2015-07-09

    申请号：US14419297

    申请日：2012-08-03

    申请人： Thomas Giller

    发明人： Thomas Giller

    IPC分类号： A61K47/02 ,  A61K47/10 ,  B65D85/00 ,  A61K47/14 ,  A61K47/06 ,  A61K45/06 ,  A61K31/357 ,  A61K47/20

    CPC分类号： A61K47/02 ,  A61K9/0019 ,  A61K31/165 ,  A61K31/335 ,  A61K31/357 ,  A61K45/06 ,  A61K47/06 ,  A61K47/10 ,  A61K47/14 ,  A61K47/20 ,  B65D85/70

    摘要： The invention relates to a resiniferatoxin solution having an enhanced storage stability, in which the resiniferatoxin is dissolved in a body-compatible solvent which contains a protective gas in solution, wherein the amount of the protective gas is at least 1 wt % of the saturation amount of the protective gas in the solvent at ambient temperature and normal pressure. The resiniferatoxin dissolved in the resiniferatoxin solution remains stable for a relatively long period and exhibits a reduced tendency to cling to polymeric surfaces.

    摘要翻译： 本发明涉及具有增强的储存稳定性的树脂毒素溶液，其中树脂毒素溶解在溶液中含有保护气体的与体内相容的溶剂中，其中保护气体的量为饱和量的至少1重量％ 的保护气体在溶剂中在环境温度和常压下进行。 溶解在树脂毒素溶液中的树脂毒素毒素保持稳定相当长的时间，并且表现出降低粘附到聚合物表面的倾向。